Protease Activated Receptor (PAR) Inhibitor

PPACK TFA is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK TFA specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK TFA exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK TFA binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK TFA is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.

FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.

Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC₅₀ of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.

GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca²⁺ release with an IC₅₀ of 2 μM.

I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gα_q and Gα_12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research.

PPACK dihydrochloride is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK dihydrochloride specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK dihydrochloride exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK dihydrochloride binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK dihydrochloride is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC₅₀=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC₅₀=0.16 μM) and thrombin (IC₅₀=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.

FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.

CBK289001 is a tartrate-resistant acid phosphatase (TRAP/ACP5) inhibitor. CBK289001 inhibits TRAP 5b^MV, TRAP 5b^OX and TRAP 5a^OX with IC₅₀s of 125 µM, 4.21 µM and 14.2 µM, respectively.

Activated protein C is an anticoagulant targeting coagulation factors Va and VIIIa. Activated protein C demonstrates cytoprotective effects through binding to endothelial cell protein C receptor (EPCR) and protease-activated receptor-1 (PAR-1), regulating gene expression, anti-inflammation, anti-apoptosis, and stabilizing endothelial barriers. Activated protein C is promising for research of diseases such as severe sepsis and ischemic stroke.

APC 366 (TFA) is an irreversible mast cell tryptase inhibitor. APC 366 (TFA) can be used for the research of allergic diseases.

Anti-PAR1 Antibody is an anti-PAR1 antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

KLK5-IN-1 is a selective kallikrein 5 (KLK5) inhibitor with an IC₅₀ of 14 nM and a K_i of 11 nM. KLK5-IN-1 reduces KLK5-mediated PAR2-dependent calcium mobilization. KLK5-IN-1 improves epithelial barrier integrity. KLK5-IN-1 can be used in research related to atopic dermatitis and Netherton syndrome.

PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC₅₀ of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T_1/2 of 42.5 min.

PC8 is a selective dual inhibitor of PARP1/CDK6, with an IC₅₀ of 0.126 μM for PARP1 and 0.197 μM for CDK6. PC8 does not alter PARP1 expression, but reduces the expression of its downstream target PAR. PC8 inhibits the canonical Wnt/β-catenin signaling pathway. PC8 induces intracellular ROS accumulation and exacerbates DNA damage. PC8 inhibits the proliferation of triple-negative breast cancer (TNBC) cells. PC8 can be used for the research of triple-negative breast cancer.

PPACK is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.

PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC₅₀ of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T_1/2 of 97.6 min.

RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC₅₀=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC₅₀=0.16 μM) and thrombin (IC₅₀=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.

ML161 analog 1 (compound 38) is an analog of ML161 (HY-13965). ML161 analog 1 is a selective allosteric inhibitor of PAR1 with an IC₅₀ of 1.68 μM.

TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC₅₀ values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner.